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Cat. No.: HY-182497

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U 95133

U 95133 is a non-nucleoside reverse transcriptase inhibitor. U 95133 exhibits activity against both wild-type and mutant HIV-1 reverse transcriptase. U 95133 can be used in studies related to HIV infection.

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CAS No.: 177577-59-2
Formule: C₂₅H₃₄N₆O₃S
Masse moléculaire:498.64

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Please store the product under the recommended conditions in the Certificate of Analysis.

U 95133 Chemical Structure

CAS No.: 177577-59-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform HIV :

In Vitro

U 95133 (compound 16) (0-100 μM) potently inhibits wild-type HIV-1 reverse transcriptase, with an IC₅₀ of 2.2 μM and an inhibition rate of 98% at a concentration of 100 μM^[1].
U 95133 potently inhibits HIV-1 replication in human peripheral blood mononuclear cells, with an ED₅₀ of <0.0001 μM^[1].
U 95133 (10 minutes) exhibits an IC₅₀ of 0.50 μM against wild-type HIV-1 reverse transcriptase, an IC₅₀ of 1.5 μM against HIV-1 reverse transcriptase ^P236L, and an IC₅₀ of 1.1 μM against HIV-1 reverse transcriptase ^Y181C^[1].
U 95133 (4 days) potently inhibits the replication of wild-type HIV-1_IIIB in MT4 cells with an IC₉₀ of 0.02 μM, and exhibits submicromolar activity against a variety of NNRTI-resistant HIV-1 variants^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

U 95133 (15 mg/kg; i.v.; p.o.) exhibits high intravenous clearance and low oral bioavailability in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 177577-59-2
Masse moléculaire 498.64
Formule C₂₅H₃₄N₆O₃S
SMILES

O=C(N1CCC(CC1)N(C)C2=NC=CC=C2NC(C)(C)C)C3=CC4=C(N3)C=CC(NS(=O)(C)=O)=C4
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Genin MJ, et al. Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs. J Med Chem. 1996;39(26):5267-5275. [Content Brief]

[2]. Olmsted R A, et al. (Alkylamino) piperidine bis (heteroaryl) piperizine analogs are potent, broad-spectrum nonnucleoside reverse transcriptase inhibitors of drug-resistant isolates of human immunodeficiency virus type 1 (HIV-1) and select for drug-resistant variants of HIV-1IIIB with reduced replication phenotypes. Journal of virology, 1996, 70(6): 3698-3705.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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U 95133

Voir tous les produits spécifiques à Isoform HIV